PF-04802367

SKU: orb1297983

Description

PF-04802367 is a potent and selective dual inhibitor of GSK-3α and GSK-3β, exhibiting low nanomolar IC₅₀ values. Its favorable CNS properties make it a valuable research tool for investigating GSK-3's role in neurological diseases, tauopathies, and mood disorders in both cellular and animal models.

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	1962178-27-3
MW	361.78
Purity	98.76% (May vary between batches)
Formula	C₁₆H₁₆ClN₅O₃
SMILES	COc1ccc(cc1Cl)-c1ocnc1C(=O)NCCCn1cncn1
Target	GSK-3
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.06 mM);DMSO:100 mg/mL (276.41 mM)

Bioactivity

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Target IC50	GSK-3α:10 nM (IC50)\|GSK-3β:9 nM (IC50)
In Vivo	PF-04802367 (PF-367) is a potent type-I dual GSK-3α/β inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels in vivo. It demonstrates dose-dependent inhibition of tau phosphorylation in the brain at subcutaneous doses of 1, 3.2, 10, 32, or 50 mg/kg. Additionally, PF-367 exhibits promising ADME properties, and robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo. Read more...
In Vitro	PF-04802367 (PF-367) effectively inhibits GSK-3β enzymatic activity in vitro, with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively . It exhibits reasonable in vitro stability in human hepatic microsomes (t1/2=78.7 min) and has excellent passive permeability . In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibits phosphorylation of tau with an IC50 of 466 nM . PF-367 demonstrates good cell viability (IC50 of 117 μM in THLE cytotoxicity assays) and an IC50 >100 μM in a hERG screening assay . It shows significant right shifts against β-catenin translocation in HeLa cells with an EC50 of 6.2 μM, gene transcription in U2OS cells with an EC50 of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with an EC50 of 9.0 μM . Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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tau, synthase, protein, PF367, PF-367, PF04802367, PF-04802367, PF 367, PF 04802367, phosphorylation, Alzheimer, disease, inhibit, kinase-3, neurodegenerative, neurology, Inhibitor, Glycogen synthase kinase-3, Glycogen, Glycogen synthase kinase 3, GSK3, GSK-3, GSK-3α/β

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Compound Identifiers

PubChem CID

60148521 ↗

Key Properties

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No computed properties available.

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PF-04802367

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Compound Identifiers

Key Properties

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PF-04802367 (orb1297983)

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